van Steen B J, van Wijngaarden I, Ronken E, Soudijn W
Solvay Pharmaceuticals Research Laboratories, Weesp, The Netherlands.
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2457-62. doi: 10.1016/s0960-894x(98)00406-5.
The agonistic/antagonistic profile of a series of 10 N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines is evaluated in the in vitro adenylyl cyclase assay. The profile is severely affected by the characteristics of the N4-substituents ranging from full agonism (benzamidoethyl derivative 1), mixed agonism/antagonism (phthalimidobutyl derivative 7) to predominantly antagonism (saccharinbutyl derivate 9). A novel full antagonist 10, as potent as WAY 100635, is obtained by substitution of Cl at C-7 of the benzodioxinyl moiety in 9.
